Global ETD Search
Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
Results
Showing 1 to 20 of 30 for “"deoxycytidine"”.
-
Synthesis of Novel 5-Aryl 2’-Deoxyuridine and 2’-Deoxycytidine Analogues
… details a synthetic route to prepare 5-phenyl-2’-deoxycytidine analogues. This multistep synthesis began with silyl protection of the 3’- and 5’-hydroxyl groups of 5-iodo-2’-deoxyuridine. Next, the installation of a phenyl ring at the C5 position of the nucleobase via a Suzuki-Miyaura …
-
Toxicological and Pharmacological Studies on Amide Derivatives of 5-Methoxymethyl-2'-Deoxycytidine
… of viral infections. Our hypothesis was that deoxycytidine analogs should have lower toxicity profile, because these pharmacophores would act selectively on virus infected cells. The antiviral activity of amide derivatives of 5-Methoxymethy1-2i-deoxycytidine (MMdCyd), namely, acetyl-MMdCyd, …
-
DEVELOPMENT OF 4'-ETHYNYL-2'-DEOXYCYTIDINE (EdC), A REPLICATION-STRESS INDUCING NUCLEOSIDE ANALOG PRODRUG WITH PREFERENTIAL ACTIVITY IN LEUKEMIA AND LYMPHOMA SUBTYPES
… screening approach, we discovered 4’-ethynyl-2’-deoxycytidine (EdC) as a third-generation anticancer nucleoside prodrug with preferential activity against diffuse large B-cell lymphoma (DLBCL) and acute lymphoblastic leukemia (ALL). EdC requires deoxycytidine kinase (dCK) phosphorylation for its …
-
Spectroscopic analysis and synthesis of nucleoside analogs for lethal mutagenesis
… nucleoside analog, 5-Aza-5,6-dihydro-2'- deoxycytidine (KP1212), employs the mechanism of lethal mutagenesis to avoid the problem of drug resistance and use the virus's high mutation rate against it. KP1212 is incorporated into DNA by HIV reverse transcriptase (RT) but mispairs with …
-
The Analysis of the MCF7 Cancer Model System and the Effects of 5-AZA-2'-Deoxycytidine Treatment on the Chromantin State Using a Novel Microarray-Based Technology for High Resolution Global Chromatin State Measurement
A microarray method to measure the global chromatin state of the human genome was developed in order to provide a novel view of gene regulation. The 'chromatin array' employs traditional methods of chromatin isolation, microarray technology, and advanced data analysis, and was applied to a cancer …
-
Studies On The Determinants Of HIV Mutagenesis And Strategies For Its Enhancement
… HIV-1 mutagenesis after reduction to 5-aza-2’-deoxycytidine (i.e. decitabine); 4) the anti-HIV-1 activity of 5-azacytidine is antagonized by inhibitors of ribonucleotide reductase; 5) the anti-HIV-1 activity of ribonucleotide reductase inhibitors are potentiated by …
-
Exposures and the Impacts on the Epigenome that Persist from Youth to Adulthood and Intergenerationally
… arsenic and the chemotherapeutic drug 5-aza-2'-deoxycytidine (Decitabine), both of which disrupt different elements of the DNA methylation pathway resulting in persistent epigenetic changes. I first share my findings on the impacts of maternal arsenic exposure, which disrupts the 1-carbon …
-
Investigations of the inhibition mechanisms of human ribonucleotide reductase by gemcitabine-5'-diphosphate and saccharomyces cerevisiae ribonucleotide reductase by Sml1
… in DNA repair. Gemcitabine (2',2'-difluoro-2'-deoxycytidine, F2C) is used clinically in a variety of cancer treatments and the phosphorylated F2C targets many enzymes involved in nucleotide metabolism, including RNR. The studies presented here with [1 '-3H]- and [5- 3H]-F 2CDP have established …
-
Remaining Unperturbed by the Vibrational Response: Probing Vibrational Coupling, Relaxation, and Solvent Effects with 2D IR Spectroscopy
… of a cyanamide vibrational probe placed onto a deoxycytidine nucleoside are investigated in a variety of viscous environments. This study not only reveals the relationship between the FFCF decay of the NCN reported and solvent viscosity, but further correlates the decay time directly with the …
-
Pathway Profiling Of Replicative And Induced Senescence
… various drugs to induce senescence: 5-aza-2-deoxycytidine (a demethylating agent), Adriamycin (a chemotherapeutic drug), and H2O2 (an agent causing oxidative stress).</p> <p>MDAH041 cells, which are fibroblasts isolated from a patient with Li Fraumeni Syndrome, have heterozygous alleles of …
-
p53 acts to prevent the formation of pathological R-loops during epigenetic stress
5-Azacytidine (Aza) and 5-Aza-2’-deoxycytidine (Dac) are the two primary therapeutics for the treatment of Acute Myeloid Leukaemia and some myelodysplastic syndromes. The two are frequently used interchangeably, surprisingly as their selectivity of de-methylation is unique from the other, however …
-
Investigating the molecular dynamics of gene re-silencing following treatment with epigenetic therapies
… DNA hypomethylating agents such as 5-Aza-2’deoxycytidine (5-Aza-dC) are approved for the treatment of myelodysplastic syndrome and show promise in the treatment of solid tumours. These therapies are thought to exert their anti-tumour effects by reactivating hypermethylated genes. However, …
-
Functional consequences of cytosine methylation in mitochondrial DNA catalyzed by DNA methyltransferase 1
… inhibition by the nucleoside analog 5-aza-2’-deoxycytidine (5-aza-dC). NRF1 and PGC1α, transcription factors that activate nuclear-encoded mitochondrial proteins in response to oxidative stress, were observed to up-regulate expression of mtDNMT1. Loss of p53, a tumor suppressor gene known to …
-
Identification and Characterization of Drug Targets in the Pyrimidine and Purine Pathways of Trypanosoma brucei
… synthesized cytosine deoxynucleotides into the deoxycytidine, which is ultimately converted to thymine deoxynucleotides. The vital role for TK in bridging pyrimidine nucleotide pools may represent a shared vulnerability unique to kinetoplastids, providing an opportunity to target multiple human …
-
DNA Triplexes in chemistry biology and medicine
… is a novel method for the synthesis of the deoxycytidine analogue, 2-amino-3-methyl-5-(2’-deoxy-?-D-ribofuranosyl)pyridine (MeP). The phosphoramidite monomer of MeP was synthesised and incorporated as a “protonated” cytidine analogue into triplex forming oligonucleotides (TFOs). It was …
-
Aberrant epigenetics in the molecular pathogenesis of human acute myeloid leukemia
… Treatment with the cytosine analog 5-Aza-2’-deoxycytidine (5-Aza-dC) in vitro resulted in promoter demethylation and p15 mRNA re-expression, which was associated with a release of a transcriptionally repressive complex at the p15 promoter. Importantly, 5-Aza-dC treatment also reversed …
-
Chronic Hypoxia Induces Epigenetic Modifications in the Fetal Rat Heart
… of the DNA methylation inhibitor, 5-aza-2-deoxycytidine, binding of SP1 to PKCε promoter, promoter methylation, and PKCε protein and mRNA were restored to control levels. Connecting epigenetics to chronic hypoxia in utero led us to further investigate the underlining mechanism of …
-
Regulation of Matrix Metalloproteinases and Their Inhibitors by DNA Methylation in Human Gestational Tissues
… treated with the demethylating agent 5-aza-2'-deoxycytidine (AZA) and/or lipopolysaccharide (LPS). qRT-PCR and western blotting revealed synergistic up-regulation of MT1-MMP and TIMP-1, by combined AZA+LPS treatments. Secreted MMP-2 and -9 activities were evaluated by gelatin zymography and …
-
COMBINATORIAL MOLECULAR PHARMACOLOGICAL AND PRECLINICAL STUDIES OF AN EPIGENETIC ANTICANCER DRUG, 3-DEAZANEPLANOCIN A, IN RATS
… agents trichostatin A (TSA) and 5-Aza-2¿-deoxycytidine (AZA), were used to probe the role of EZH2 in coordination with other epigenetic components in gene regulation in breast cancer cells and to identify a comprehensive set of genes functionally enriched in inflammation network and …
Page 1 of 2